中药鸡血藤质量控制与体内代谢研究
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摘要
鸡血藤是我国的传统中药,具有补血、活血、通络之传统功效,一般用于治疗月经不调、血虚萎黄、麻木瘫痪、风湿痹痛等症。迄今为止,对于该中药的研究不少,但大多数只停留在化学成分和药理作用方面的研究。为了深入阐明该药的作用物质基础并建立该药与疗效相关的质量控制方法,本课题对鸡血藤的化学成分、指纹图谱、药物代谢动力学和含量测定进行了系统的研究。
采用溶剂法和各种色谱技术对鸡血藤乙醇提取物的化学成分进行了研究,从该植物中共分离得到31个化合物。并应用波谱技术对上述化合物进行了结构鉴定,其中包括22个黄酮类化合物,2个木脂素,7个其他类型的化合物。其中有18化合物个首次从该植物中分离得到。
建立了HPLC指纹图谱分析方法及相关软件分析,成功应用于29批不同收集地鸡血藤的质量控制。采用相似度评价软件,聚类分析和主成分分析,对29批药材进行了分类、评价;通过与对照品比较,指认了19个成份,从而能够全面、可靠地反映鸡血藤药材的质量。
首次选择(2R,3R)-3,7-dihydroxyflavanone, (2R,3R)-buteaspermanol和formononetin为指标性成分,采用LC/MS (MRM)研究了鸡血藤提取物在大鼠体内药物代谢动力学,并用药时曲线描述了此类化合物的动态吸收过程。这可以为鸡血藤及鸡血藤相关制剂的体内作用机理的简述和临床合理用药提供有价值的参考。
应用HPLC-DAD和HPLC-ESI-MS/MS技术建立了鸡血藤药材中7个有效成成分同时定量研究的方法,并成功地应用于14批鸡血藤药材的质量控制。该分析方法简单、快速、准确,可以为鸡血藤药材及含鸡血藤制剂的质量标准制定提供参考。
Spatholobus suberectus Dunn is a traditional Chinese medicine. It has traditional efficacy of enrichment the blood, promoting blood circulation and activating collaterals, which is generally used in the treatment of menstruation, hemopenia yellow, numbness paralysis, rheumatism bi-complex pain and so on. So far, the research of S. suberectus was still inadequate. In order to further elucidate the significant role of the above herbal medicine and establish its scientific quality control method, the chemical constituents, fingerprint, pharmacokinetic and simultaneous determination of multiple bioactive constituents of the above herbal medicine were systematically investigated.
The ethanol extracts of the S. suberectus were chemically investigated by various chromatography methods. As a result, 31 compounds were isolated from the title plant. Their structures were characterized by chemical and spectroscopic methods, including 22 flavonoids, 2 lignans and 7 other types of compounds, 18 of which were isolated from this plant for the first time.
The HPLC fingerprint analysis method were established and successfully applied to 29 batches of S. suberectus samples collected from different provices for the quality control. Using similarity evaluation software, cluster analysis and principal component analysis, 29 batches of S. suberectus samples were classified and evaluated. Compared with reference substances, 19 components were identified, which can be comprehensively reliable to reflect the qualities of S. suberectus.
Pharmacokinetics in rats were investigated by LC/MS (MRM) after oral administration of the total extract of S. suberectus. (2R,3R)-3,7-Dihydroxyflavanone, (2R,3R)-buteaspermanol and formononetin were choosed as indicative composition. The concentration–time curves described dynamic absorption process of the above type of compounds. This can provide valuable reference for the exploration of activity mechanism and clinically use of S. suberectus and its related preparations.
The analysis methods (HPLC-DAD and HPLC-ESI-MS/MS) were applied successfully in the quantitative analysis of 7 main bioactive components in 14 batches S. suberectus samples. The method was proved to be simple, rapid and accurate. It can provide standard reference for the quality control of the S. suberectus and the preparations containing S. suberectus.
采用溶剂法和各种色谱技术对鸡血藤乙醇提取物的化学成分进行了研究,从该植物中共分离得到31个化合物。并应用波谱技术对上述化合物进行了结构鉴定,其中包括22个黄酮类化合物,2个木脂素,7个其他类型的化合物。其中有18化合物个首次从该植物中分离得到。
建立了HPLC指纹图谱分析方法及相关软件分析,成功应用于29批不同收集地鸡血藤的质量控制。采用相似度评价软件,聚类分析和主成分分析,对29批药材进行了分类、评价;通过与对照品比较,指认了19个成份,从而能够全面、可靠地反映鸡血藤药材的质量。
首次选择(2R,3R)-3,7-dihydroxyflavanone, (2R,3R)-buteaspermanol和formononetin为指标性成分,采用LC/MS (MRM)研究了鸡血藤提取物在大鼠体内药物代谢动力学,并用药时曲线描述了此类化合物的动态吸收过程。这可以为鸡血藤及鸡血藤相关制剂的体内作用机理的简述和临床合理用药提供有价值的参考。
应用HPLC-DAD和HPLC-ESI-MS/MS技术建立了鸡血藤药材中7个有效成成分同时定量研究的方法,并成功地应用于14批鸡血藤药材的质量控制。该分析方法简单、快速、准确,可以为鸡血藤药材及含鸡血藤制剂的质量标准制定提供参考。
Spatholobus suberectus Dunn is a traditional Chinese medicine. It has traditional efficacy of enrichment the blood, promoting blood circulation and activating collaterals, which is generally used in the treatment of menstruation, hemopenia yellow, numbness paralysis, rheumatism bi-complex pain and so on. So far, the research of S. suberectus was still inadequate. In order to further elucidate the significant role of the above herbal medicine and establish its scientific quality control method, the chemical constituents, fingerprint, pharmacokinetic and simultaneous determination of multiple bioactive constituents of the above herbal medicine were systematically investigated.
The ethanol extracts of the S. suberectus were chemically investigated by various chromatography methods. As a result, 31 compounds were isolated from the title plant. Their structures were characterized by chemical and spectroscopic methods, including 22 flavonoids, 2 lignans and 7 other types of compounds, 18 of which were isolated from this plant for the first time.
The HPLC fingerprint analysis method were established and successfully applied to 29 batches of S. suberectus samples collected from different provices for the quality control. Using similarity evaluation software, cluster analysis and principal component analysis, 29 batches of S. suberectus samples were classified and evaluated. Compared with reference substances, 19 components were identified, which can be comprehensively reliable to reflect the qualities of S. suberectus.
Pharmacokinetics in rats were investigated by LC/MS (MRM) after oral administration of the total extract of S. suberectus. (2R,3R)-3,7-Dihydroxyflavanone, (2R,3R)-buteaspermanol and formononetin were choosed as indicative composition. The concentration–time curves described dynamic absorption process of the above type of compounds. This can provide valuable reference for the exploration of activity mechanism and clinically use of S. suberectus and its related preparations.
The analysis methods (HPLC-DAD and HPLC-ESI-MS/MS) were applied successfully in the quantitative analysis of 7 main bioactive components in 14 batches S. suberectus samples. The method was proved to be simple, rapid and accurate. It can provide standard reference for the quality control of the S. suberectus and the preparations containing S. suberectus.
引文
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